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前体蛋白转化酶抑制剂潜在的抗肿瘤和抗转移作用

The potential anti-tumorigenic and anti-metastatic side of the proprotein convertases inhibitors.

作者信息

Lahlil Rachid, Calvo Fabien, Khatib Abdel-Majid

机构信息

INSERM, U 716, Equipe Avenir. Institut de Génétique Moléculaire, Paris, 75010, France.

出版信息

Recent Pat Anticancer Drug Discov. 2009 Jan;4(1):83-91. doi: 10.2174/157489209787002470.

Abstract

The setup of tumorigenesis processes is generally associated with various events leading to abnormal expression of oncogenes and/or tumor suppressor genes. Recently, the expression and/or activity of a range of molecules involved in these processes were reported to require proteolytic processing of their precursor proteins by the serine pro-protein convertases (PCs) in order to mediate their biological functions. These include adhesion molecules, proteases, growth factors, cytokines and their receptors. Since their discovery, the identification of new PCs substrates and specific PCs inhibitors became an attractive strategy in cancer therapy. In this review, we will report the implication of these enzymes and the processing of their substrates in tumor progression and metastasis. Newly reported studies on the potential use of the PCs as new therapeutic targets will be also discussed.

摘要

肿瘤发生过程的建立通常与导致癌基因和/或肿瘤抑制基因异常表达的各种事件相关。最近,据报道,参与这些过程的一系列分子的表达和/或活性需要丝氨酸前体蛋白转化酶(PCs)对其前体蛋白进行蛋白水解加工,以介导其生物学功能。这些分子包括黏附分子、蛋白酶、生长因子、细胞因子及其受体。自发现以来,鉴定新的PCs底物和特异性PCs抑制剂已成为癌症治疗中一种有吸引力的策略。在本综述中,我们将报告这些酶及其底物的加工在肿瘤进展和转移中的作用。还将讨论关于将PCs用作新治疗靶点的潜在用途的最新报道研究。

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